Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Gerard R, Kieczykowski"'
Autor:
Gerard R. Kieczykowski, Carrie P. Jones, Ping Liu, Junying Wang, Conrad E. Raab, Qian Si, Xinchun Tong, Thomas J. Lanza, Anne Schuelke, Kelly M. Treonze, Richard A. Mumford, Salony Manior, Stella H. Vincent, James V. Pivnichny, Gloria C. Koo, James P. Jewell, William K. Hagmann, Regina W. Wang, Philip Davies, Linus S. Lin, Malcolm MacCoss
Publikováno v:
Journal of Medicinal Chemistry. 52:3449-3452
Extremely potent very late antigen-4 (VLA-4) antagonists with picomolar, whole blood activity and slow dissociation rates were discovered by incorporating an amino substituent on the proline fragment of the initial lead structure. This level of poten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3a2b44376091abb5e0b00c51b9e55a39
https://doi.org/10.1021/jm900257b
https://doi.org/10.1021/jm900257b
Autor:
Karen Marcantonio, Enrique Vazquez, Cheng-yi Chen, Lisa F. Frey, Joeseph F. Payack, Scott Shultz, Jeff Strine, George Zhou, Ping Liu, Shawn A. Springfield, Debra J. Wallace, Alex M. Chen, Brian D. Phenix, and Brianne Izzo, Gerard R. Kieczykowski, Utpal K. Singh, Shane W. Krska
Publikováno v:
Organic Process Research & Development. 11:616-623
Chiral amide 1 (MK-0364, taranabant) is a potent, selective, and orally bioavailable cannabinoid-1 receptor (CB-1R) inverse agonist indicated for the treatment of obesity. An asymmetric synthesis featuring a dynamic kinetic resolution via hydrogenati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3be255de6dd8e40770c08d25ef925f52
https://doi.org/10.1021/op700026n
https://doi.org/10.1021/op700026n
Autor:
Huaibing He, George J. Eiermann, Nancy A. Thornberry, Dennis Feng, Bei Zhang, Xiaoping Zhang, Tesfaye Biftu, Suresh B. Singh, Ranabir SinhaRoy, Kathy Lyons, Ann E. Weber, Ying-Duo Gao, Joseph K. Wu, Barbara Leiting, Gui-Bai Liang, Sangita B. Patel, Aleksandr Petrov, Xiaoxia Qian, Gerard R. Kieczykowski, Giovanna Scapin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:49-52
Replacement of the triazolopiperazine ring of sitagliptin (DPP-4 IC50 = 18 nM) with 3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one gave dipeptidyl peptidase IV (DPP-4) inhibitor 1 which is potent (DPP-4 IC50 = 2.6 nM), selective, and efficacious in an o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90c3e0b3be6396416a385fb7d2aa8c88
https://doi.org/10.1016/j.bmcl.2006.09.099
https://doi.org/10.1016/j.bmcl.2006.09.099
Publikováno v:
Synthesis. 2007:2779-2781
A short, high yielding, five-step synthesis of the pharmaceutically interesting fluorinated heterocycle, 3-[2,2,2-trifluoroethyl]hexahydro-2 H-1,4-diazepin-2-one, has been developed.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9d6453cd58596fbe31841fe707ac6c08
https://doi.org/10.1055/s-2007-983876
https://doi.org/10.1055/s-2007-983876
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1401-1404
Screening of our sample collection for novel structures with endothelin receptor (ET A and ET B ) binding affinity, resulted in the discovery of structure I (R = H). This unique bicyclic diacid elicited modest affinity for both cloned human receptors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3225eefda02a2ac3701c0890ff7252fd
https://doi.org/10.1016/0960-894x(95)00230-q
https://doi.org/10.1016/0960-894x(95)00230-q
Autor:
Richard Hajdu, Joan M. Pierce, Russell B. Lingham, Carol Ann Keohane, Vincent J. Colandrea, Lisa M. Sonatore, Dietrich Steinhuebel, James A. Milligan, Jeffrey J. Hale, Can D Akyuz, Fred J. Fleitz, Julie A. DeMartino, Suzanne M. Mandala, Michael Wolff, Dhirendra K Jena, John Athanasopoulos, Juncai Meng, Edward C. Sherer, Petr Vachal, Kevin T. Chapman, Jeffrey W. Lusen, Gerard R. Kieczykowski, Scott P. Salowe, Gregory C. Adam, Xinchun Tong, Benjamin D. Stein, Shouwu Miao, Anantha Gollapudi, Lei Xia, Deodial Guiadeen, Matthew J. Wyvratt
Publikováno v:
Journal of medicinal chemistry. 55(7)
The discovery of 1,3,8-triazaspiro[4.5]decane-2,4-diones (spirohydantoins) as a structural class of pan-inhibitors of the prolyl hydroxylase (PHD) family of enzymes for the treatment of anemia is described. The initial hit class, spirooxindoles, was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ebfa041b8e71a1b6ca8c48a2bfea0fad
https://pubmed.ncbi.nlm.nih.gov/22409479
https://pubmed.ncbi.nlm.nih.gov/22409479
Autor:
Linus S, Lin, Thomas, Lanza, James P, Jewell, Ping, Liu, Carrie, Jones, Gerard R, Kieczykowski, Kelly, Treonze, Qian, Si, Salony, Manior, Gloria, Koo, Xinchun, Tong, Junying, Wang, Anne, Schuelke, James, Pivnichny, Regina, Wang, Conrad, Raab, Stella, Vincent, Philip, Davies, Malcolm, Maccoss, Richard A, Mumford, William K, Hagmann
Publikováno v:
Journal of medicinal chemistry. 52(11)
Extremely potent very late antigen-4 (VLA-4) antagonists with picomolar, whole blood activity and slow dissociation rates were discovered by incorporating an amino substituent on the proline fragment of the initial lead structure. This level of poten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::e9a6bbef5a020db297b6f1e1be61f223
https://pubmed.ncbi.nlm.nih.gov/19441819
https://pubmed.ncbi.nlm.nih.gov/19441819
Publikováno v:
ChemInform. 39
A short, high yielding, five-step synthesis of the pharmaceutically interesting fluorinated heterocycle, 3-[2,2,2-trifluoroethyl]hexahydro-2 H-1,4-diazepin-2-one, has been developed.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c23a0957dfd0e8637b540debfd99d66c
https://doi.org/10.1002/chin.200807147
https://doi.org/10.1002/chin.200807147
Autor:
Mark T. Goulet, Rosemary Sisco, Xiaolan Shen, Jisong Cui, An-Hua Mao, Bindhu V. Karanam, Kang Cheng, Gerard R. Kieczykowski, Tsuei-Ju Wu, Kathryn A. Lyons, Rena Ning Ren, Stella H. Vincent, George R. Mount, Yi Tien Yang, Josephine R. Carlin, Wallace T. Ashton, Joel B. Yudkovitz
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(19)
Stereospecific introduction of a methyl group to the indole-3-side chain enhanced activity in our tryptamine-derived series of GnRH receptor antagonists. Further improvements were achieved by variation of the bicyclic amino moiety of the tertiary ami
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62aa10fe83ceeb8e6e55192fca6d7d38
https://pubmed.ncbi.nlm.nih.gov/11551758
https://pubmed.ncbi.nlm.nih.gov/11551758
Autor:
Linus S. Lin, Thomas Lanza, James P. Jewell, Ping Liu, Carrie Jones, Gerard R. Kieczykowski, Kelly Treonze, Qian Si, Salony Manior, Gloria Koo, Xinchun Tong, Junying Wang, Anne Schuelke, James Pivnichny, Regina Wang, Conrad Raab, Stella Vincent, Philip Davies, Malcolm MacCoss, Richard A. Mumford
Publikováno v:
Journal of Medicinal Chemistry; Jun2009, Vol. 52 Issue 11, p3449-3452, 4p